Cited by 119Cannabis and Cannabinoid ResearchPain Mechanisms and TreatmentsIon Channels and Receptors

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The fatty acid amide hydrolase (FAAH) inhibitor PF‐3845 acts in the nervous system to reverse LPS‐induced tactile allodynia in mice

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Booker, Lamont, Kinsey, Steven G, Abdullah, Rehab A, Blankman, Jacqueline L, Long, Jonathan Z, Ezzili, Cyrine, Boger, Dale L, Cravatt, Benjamin F, Lichtman, Aron H·2012·British Journal of Pharmacology

DOI 10.1111/j.1476-5381.2011.01445.xPMC PMC3423256

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Abstract

BACKGROUND AND PURPOSE Inflammatory pain presents a problem of clinical relevance and often elicits allodynia, a condition in which non‐noxious stimuli are perceived as painful. One potential target to treat inflammatory pain is the endogenous cannabinoid (endocannabinoid) system, which is comprised of CB 1 and CB 2 cannabinoid receptors and several endogenous ligands, including anandamide (AEA). Blockade of the catabolic enzyme fatty acid amide hydrolase (FAAH) elevates AEA levels and elicits antinociceptive effects, without the psychomimetic side effects associated with Δ 9‐tetrahydrocannabinol (THC). EXPERIMENTAL APPROACH Allodynia was induced by intraplantar injection of LPS. Complementary genetic and pharmacological approaches were used to determine the strategy of blocking FAAH to reverse LPS‐induced allodynia. Endocannabinoid levels were quantified using mass spectroscopy analyses. KEY RESULTS FAAH (−/−) mice or wild‐type mice treated with FAAH inhibitors (URB597, OL‐135 and PF‐3845) displayed an anti‐allodynic phenotype. Furthermore, i.p. PF‐3845 increased AEA levels in the brain and spinal cord. Additionally, intraplantar PF‐3845 produced a partial reduction in allodynia. However, the anti‐allodynic phenotype was absent in mice expressing FAAH exclusively in the nervous system under a neural specific enolase promoter, implicating the involvement of neuronal fatty acid amides (FAAs). The anti‐allodynic effects of FAAH‐compromised mice required activation of both CB 1 and CB 2 receptors, but other potential targets of FAA substrates (i.e. µ‐opioid, TRPV1 and PPARα receptors) had no apparent role. CONCLUSIONS AND IMPLICATIONS AEA is the primary FAAH substrate reducing LPS‐induced tactile allodynia. Blockade of neuronal FAAH reverses allodynia through the activation of both cannabinoid receptors and represents a promising target to treat inflammatory pain. LINKED ARTICLES This article is part of a themed section on Cannabinoids in Biology and Medicine. To view the other articles in this section visit http://dx.doi.org/10.1111/bph.2012.165.issue‐8. To view Part I of Cannabinoids in Biology and Medicine visit http://dx.doi.org/10.1111/bph.2011.163.issue‐7

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“PF-3845 LPS model of inflammatory pain Anti-allodynic Booker et al. (2012)”
BackgroundMethodInfluential
Role of FAAH-Like Anandamide Transporter in Anandamide Inactivation
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“…was chosen on the basis of previous published work which demonstrated that systemic administration of PF3845 increased brain levels of the FAAH substrates AEA, OEA and induced biological effects in several assays (Ahn et al, 2009; Booker et al, 2012; Nasirinezhad et al, 2015; Rock et al, 2015).”
Method
FAAH inhibition attenuates TLR3-mediated hyperthermia, nociceptive- and anxiety-like behaviour in female rats
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α-Ketoheterocycle-Based Inhibitors of Fatty Acid Amide Hydrolase (FAAH)
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Neuroprotective effects of fatty acid amide hydrolase catabolic enzyme inhibition in a HIV-1 Tat model of neuroAIDS
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“Specifically, PF3845 increases neuronal survival, and elicits anti-nociceptive and anti-inflammatory effects in mice without cannabimimetic side effects (Booker et al., 2012; Tchantchou et al., 2014).”
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Supra-spinal FAAH is required for the analgesic action of paracetamol in an inflammatory context
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Investigation of Diacylglycerol Lipase Alpha Inhibition in the Mouse Lipopolysaccharide Inflammatory Pain Model
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“As previously reported, this is the minimally effective dose of LPS that elicits mechanical allodynia, but not measurable increases in paw thickness (Booker et al., 2012).”
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Potentiation of microglial endocannabinoid signaling alleviates neuroinflammation in Alzheimer's disease
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Endocannabinoid modulation of inflammatory hyperalgesia in the IFN-α mouse model of depression
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Protective Action of Anandamide and Its COX-2 Metabolite against l-Homocysteine-Induced NLRP3 Inflammasome Activation and Injury in Podocytes
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“…KO (Naidu et al., 2010; Kinsey et al., 2011;Wang et al., 2015), fatty acid amide hydrolase inhibitors (Kinsey et al., 2011; Schuelert et al., 2011; Booker et al., 2012; Caprioli et al., 2012; Kerr et al., 2012; Murphy et al., 2012; Sasso et al., 2012; Krustev et al., 2014; Sałaga et al., 2014;…”
Background
Evaluation of different drug classes on transient sciatic nerve injury–depressed marble burying in mice
Wilkerson, J. L., Curry, Z. A., Kinlow, P. D., Mason, B. L., Hsu, K., van der Stelt, M., Cravatt, B. F., & Lichtman, A. H. (2018) · Pain · doi:10.1097/j.pain.0000000000001199 · Cited by 27
“number of animals is sufficient for the detection of significant effects for pain-evoked behaviors.(6,29,34,36,72) To ensure reproducibility of our data, we voluntarily triplicated the morphine dose–response study, including vehicle treatment, and finding no significant differences in the sets of data, collapsed them…”
MethodSelf-citation
Inhibitory Control Deficits Associated with Upregulation of CB1R in the HIV-1 Tat Transgenic Mouse Model of Hand
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GPR18 drives FAAH inhibition-induced neuroprotection against HIV-1 Tat-induced neurodegeneration
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“FAAH inhibitors represent a promising pharmaceutical treatment for HIV-induced neurotoxicity and HAND progression given decreased FAAH activity leads to heightened levels of AEA and other anti-inflammatory fatty acid amides (Booker et al., 2012).”
BackgroundInfluentialSelf-citation
Genetic Manipulation of the Endocannabinoid System
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BackgroundSelf-citation
Identification of Fatty Acid Binding Protein 5 Inhibitors Through Similarity-Based Screening
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“A significant number of these studies indicate that endocannabinoids elicit anti-inflammatory effects.(13,32,34-37) Thus, increasing the levels of the endocannabinoids could theoretically be beneficial due to their ability to attenuate the negative effects of inflammation.”
Background
The monoacylglycerol lipase inhibitor KML29 with gabapentin synergistically produces analgesia in mice
Crowe, M. S., Wilson, C. D., Leishman, E., Prather, P. L., Bradshaw, H. B., Banks, M. L., & Kinsey, S. G. (2017) · British Journal of Pharmacology · doi:10.1111/bph.14055 · Cited by 20
“, 2009), inflammatory (Schlosburg et al., 2009; Booker et al., 2012) and visceral pain (Naidu et al.”
BackgroundSelf-citation
Endocannabinoid Signaling in the Central Amygdala and Bed Nucleus of the Stria Terminalis: Implications for the Pathophysiology and Treatment of Alcohol Use Disorder
Bedse, G., Centanni, S. W., Winder, D. G., & Patel, S. (2019) · Alcoholism Clinical and Experimental Research · doi:10.1111/acer.14159 · Cited by 19
“…efficacy of eCB degradation inhibitors without overt cannabimimetic side effects (Hruba et al., 2015, Bedse et al., 2018, Long et al., 2009, Ignatowska-Jankowska et al., 2014, Cravatt and Lichtman, 2003, Ghosh et al., 2015, Booker et al., 2012, Curry et al., 2018, Wilkerson et al., 2016).”
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The endocannabinoidomes: Pharmacological redundancy and promiscuity, and multi-kingdom variety of sources and molecular targets
Iannotti, F. A., & Marzo, V. D. (2025) · Pharmacological Reviews · doi:10.1016/j.pharmr.2025.100070 · Cited by 23
Tonic Endocannabinoid Signaling Gates Synaptic Plasticity in Dorsal Raphe Nucleus Serotonin Neurons Through Peroxisome Proliferator-Activated Receptors
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Challenging the challenge: A randomized controlled trial evaluating the inflammatory response and pain perception of healthy volunteers after single-dose LPS administration, as a potential model for inflammatory pain in early-phase drug development
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Elevating levels of the endocannabinoid 2-arachidonoylglycerol blunts opioid reward but not analgesia
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Mini-review: The therapeutic role of cannabinoids in neuroHIV
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“Additionally, the new generation of hydrolytic enzyme inhibitors, such as FAAH inhibitor PF3845 and MAGL inhibitors MJN110 and Abx-1431 show highly improved selectivity, potency and produce less side effects compared to previously available compounds [5,27,46,64,110,111,114,171,182].”
Druggable Targets in Endocannabinoid Signaling
Gregus, A. M., & Buczynski, M. W. (2020) · Advances in experimental medicine and biology · doi:10.1007/978-3-030-50621-6_8 · Cited by 16
Cannabinoids & Stress: Impact of HU-210 on behavioral tests of anxiety in acutely stressed mice
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Modulation of Pain Sensitivity by Chronic Consumption of Highly Palatable Food Followed by Abstinence: Emerging Role of Fatty Acid Amide Hydrolase
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“Thereafter, a highly selective urea-based irreversible FAAH inhibitor, PF-3845, was developed by Pfizer and shown to be an efficacious analgesic in inflammatory (Ahn et al., 2009; Booker et al., 2012) and neuropathic (Schlosburg et al., 2010) pain models.”
Background
Retracted
PF-3845, a Fatty Acid Amide Hydrolase Inhibitor, Directly Suppresses Osteoclastogenesis through ERK and NF-κB Pathways In Vitro and Alveolar Bone Loss In Vivo
Ihn, H. J., Kim, Y., Lim, S.-M., Bae, J., Jung, J., Kim, Y. H., Park, J., Wang, Z., Koh, J., Bae, Y.-C., et al. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22041915 · Cited by 13
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Method
Behavioral Battery for Testing Candidate Analgesics in Mice. II. Effects of Endocannabinoid Catabolic Enzyme Inhibitors and ∆9-Tetrahydrocannabinol
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“…antinociceptive effects of MAGL and FAAH to be CB1/2R-mediated in neuropathic and inflammatory pain models, with some inconsistencies for the involvement of CB2R in MAGL effects (Kinsey et al., 2009; Naidu et al., 2010; Booker et al., 2012; Ignatowska-Jankowska et al., 2015; Burston et al., 2016).”
BackgroundMethodInfluentialSelf-citation
A chemical genetic screen uncovers a small molecule enhancer of the N-acylethanolamine degrading enzyme, fatty acid amide hydrolase, in Arabidopsis
Khan, B. R., Faure, L., Chapman, K. D., & Blancaflor, E. B. (2017) · Scientific Reports · doi:10.1038/srep41121 · Cited by 10
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Background
Effects of R ‐flurbiprofen and the oxygenated metabolites of endocannabinoids in inflammatory pain mice models
Buisseret, B., Guillemot‐Legris, O., Kouidar, Y. B., Paquot, A., Muccioli, G. G., & Alhouayek, M. (2021) · The FASEB Journal · doi:10.1096/fj.202002468r · Cited by 11
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Maca, A Nutraceutical From the Andean Highlands
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Development of Dual Inhibitors of Soluble Epoxide Hydrolase/Fatty Acid Amide Hydrolase with Tetrazole Core
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Supraphysiological Testosterone Levels Shorten the QT Interval but do Not Alter Total Anatomic Myocardial Infarct Size in Rabbits with Acute Myocardial Infarction
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Authors: Booker, L., Kinsey, S. G., Abdullah, R. A., Blankman, J. L., Long, J. Z., Ezzili, C., Boger, D. L., Cravatt, B. F., & Lichtman, A. H.
Affiliations: Virginia Commonwealth University (US)
Scripps Research Institute (US)
Corresponding author: Lichtman, Aron H
ORCID: Kinsey, Steven G
Long, Jonathan Z
Boger, Dale L
Cravatt, Benjamin F
Lichtman, Aron H
Venue: British Journal of Pharmacology
Publisher: Wiley
Published: 2012-03-23
Volume: 165
Issue: 8
Pages: 2485-2496
ISSN: 0007-1188 (ISSN-L)
1476-5381
DOI: 10.1111/j.1476-5381.2011.01445.x
PMC: PMC3423256
OpenAlex: W1500005891
Cited by: 116
References: 49
Citations by year: 2026: 6 · 2025: 3 · 2024: 5 · 2023: 2 · 2022: 3 · 2021: 17 · 2020: 4 · 2019: 10 · 2018: 7 · 2017: 13 · 2016: 8 · 2015: 9 · 2014: 11 · 2013: 11 · 2012: 3
FWCI: 7.26
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: onlinelibrary.wiley.com/termsAndConditions#vor (vor)
Locations: British Journal of Pharmacology (publishedVersion)
Europe PMC (PubMed Central) (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Funders: National Institute on Drug Abuse (R01DA015648, P01DA009789, R01DA015683, F31DA028333, P01DA017259, R01DA003672, R01-DA-03672, P50DA005274, T32DA007027)
Topics: Health Sciences › Medicine › Pharmacology (medical) › Cannabis and Cannabinoid Research
Health Sciences › Medicine › Physiology (medical) › Pain Mechanisms and Treatments
Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
Keywords: fatty acid amide hydrolase, FAAH inhibitors, anandamide, endocannabinoid system, mechanical allodynia, inflammatory pain, lipopolysaccharide, CB1 receptor, CB2 receptor, antinociception, spinal cord, brain, URB597
MeSH terms: Fatty Acid Amide Hydrolases, Amidohydrolases, Animals, Arachidonic Acids, Brain, Enzyme Inhibitors, Female, Glycerides, Hyperalgesia, Inflammation, Lipopolysaccharides, Male, Mice, Inbred C57BL, Piperidines, Pyridines, Spinal Cord, Peripheral Nervous System, Mice, Knockout, Receptor, Cannabinoid, CB1, Receptor, Cannabinoid, CB2, Mice, Polyunsaturated Alkamides, Endocannabinoids

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The fatty acid amide hydrolase (FAAH) inhibitor PF‐3845 acts in the nervous system to reverse LPS‐induced tactile allodynia in mice

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